Categories: Hormones

PEA (phenylethylamine): Brain’s Natural Stimulant

The Brain’s Natural Stimulant for Higher Performance and Longevity

By Richard Clark Kaufman, PhD

PEA is an endogenous stimulant of the human brain that amplifies the activity of major neurotransmitters for increased longevity, slower aging, higher performance, a sense of wellbeing, and a renewed youthful-functioning body. PEA has unique rapid uplifting effects on mood, mental activity, attention, motivation, alertness, creativity, awareness, energy, stamina, physical activity, pleasurable feelings, sexuality, and sensory perceptions. PEA (beta-phenylethylamine is a naturally occurring trace amine neurotransmitter (chemical signal messenger between nerves) and neuroregulator that is normally synthesized in the brain from the amino acid phenylalanine. PEA amplifies the signal strength and effectiveness of the major neurotransmitters in the human brain to improve your life.

PEA increases the actions of dopamine (for wellbeing and feeling pleasure), norepinephrine (the brain’s stimulant for wakefulness and higher performance), acetylcholine (for improving memory and mental activity), and serotonin (for better mood emotion and impulse control). PEA is a highly-concentrated neurotransmitter in the limbic system (the brain’s emotional center) that increases motivation, physical drive, feelings, and social activity.

PEA: The Brain’s Endogenous Mesencephalic Enhancer

According to researchers, PEA is an endogenous “mesencephalic enhancer.” It plays a key role in the functioning of our innate and acquired drives. There are enhancer-sensitive neurons in the brain that work in a split second on a high activity level due to PEA. In mere microseconds, PEA causes an impulse-mediated release of catecholamines (dopamine and epinephrine) and serotonin in the brain. There are rapidly occurring improvements in cognitive performance, attention, awareness, pleasure, libido, and sense of wellbeing.

Due to the progressive decay of the mesencephalic enhancer regulation with the passing of time, the daily use of an enhancer substance like PEA during post-developmental life could significantly slow the age-related decay of behavioral performances, prolong life, and prevent the precipitation or delay the onset of Parkinson’s disease and Alzheimer’s disease.

Amplifies Neurotransmitter Signals for Peak Mental and Physical Performance at Any Age

PEA is literally a “neuro-amplifier” for higher performance in life. PEA enhances the electronic coupling in the synaptic gap between nerve cells. It boosts the signal strength of neurotransmitters by increasing their signal-to-noise ratio. This means that PEA more efficiently couples the release of neurotransmitters to the electrical impulse that triggers their release. The end result is that PEA cranks up the volume of neurotransmitter activity for higher performance throughout the body, and it does not matter how old you are to experience a noticeable performance improvement in daily activities.

Protects Sensitive Brain Circuitry

PEA protects the delicate neural circuits by preventing over-excitation or under-stimulation of neural transmissions. PEA keeps the entire system in balance and neural activity operating more efficiently and safely within dynamic limits for peak performance.

Promotes Longevity, Slower Aging, and More Youthful Functions

PEA is a powerful weapon for fighting aging. It has a unique ability to help delay aging, extend one’s healthy life span, and restore more youthful mental and physical functions. PEA improves the activity of dopamine/noradrenalin neurons, which have a pivotal role in regulating aging. According to the pioneering research of Dr. Joseph Knoll, a respected neurochemist, pharmacologist, and emeritus professor, catecholamine levels (neurotransmitters such as dopamine and norepinephrine) reach a maximum at sexual maturity and then begin a long, gradual downhill slide. The rate of decline decides how fast a person ages. According to Dr. Knoll, catecholamine levels, learning ability, sexual activity, and longevity are all interlinked.

The efficiency of your catecholamine brain machinery plays a major role in determining the quality and duration of your life. Higher-performing, longer-living individuals have a more active, more slowly deteriorating catecholamine system than their lower-performing, shorter-living peers.

By rehabilitating the brain’s catecholamine system with mesencephalic-enhancer substances (including PEA and its derivatives), it is possible to transform a lower-performing, shorter-living individual into a better-performing, longer-living one with more youthful mental and physical functions.

Starting around age 25, there is a lifelong decline in catecholamine neurotransmitters (epinephrine, norepinephrine, and dopamine), a slower decline in the indoleamine neurotransmitter (serotonin), and a shifting imbalance of the catecholamine/serotonin ratio. Catecholamine deficiencies and neurotransmitter imbalances are a principal cause of loss of “hypothalamic sensitivity” for the progressive metabolic shifts that produce aging and the diseases of aging, according to Dr. Vladimir Dilman’s Neuroendocrine Theory of Aging.

According to Dr. Dilman, a renowned Russian biogerontologist, aging is caused by a progressive loss of sensitivity by the hypothalamus (and related structures in the brain) to feedback inhibition from hormones and neurotransmitters. Throughout one’s lifespan, this loss of sensitivity produces a progressive shifting away from internal balance and altered levels of hormones, neurotransmitters, and cell signalers. These are the cause of many post-maturational diseases, accelerated aging, and earlier death. The Neuroendocrine Theory of Aging explains in detail how this causes the major diseases of aging, which contribute to over 85 percent of early deaths of middle-aged and elderly individuals.

To correct catecholamine deficiencies to help delay aging, prolong life span, prevent aging disorders, and restore youthful biological functions, Dr. Dilman and other researchers in the field of anti-aging have suggested the following:

  1. Increase neurotransmitter production and activity;
  2. Decrease catecholamine breakdown from MAO-B enzymes;
  3. Correct neurotransmitter deficiency and imbalance of the catecholamine/serotonin ratio;
  4. Inhibit neurotransmitter re-uptake, to increase inter-synaptic neurotransmitter levels; and
  5. Correct the decrease in receptor sensitivity and responsiveness of target cells and tissues to neurotransmissions.

Rehabilitates Neurotransmitter Systems That Fight Aging

PEA increases neurotransmitter production and signal activity while helping correct a neurotransmitter deficiency and imbalance of the catecholamine/serotonin ratio. PEA inhibits neurotransmitter re-uptake and regulates the responses of cells to neurotransmissions for a stable internal equilibrium. PEA is the parent compound of l-deprenyl, a catecholamine-enhancing, dopamine-increasing, and neuro-protective compound with proven life extension actions in animal research. L-deprenyl produces a huge spike in brain PEA that contributes to its anti-aging actions.

A Natural, Safe Stimulant for the Brain

PEA has invigorating, stimulating, energizing effects. PEA acts on the central nervous system to produce alertness, wakefulness, attention, energy, and endurance. Unlike drug stimulants that are highly addictive and harmful to your health, PEA is free of harmful side-effects, and is non-toxic and non-addictive. PEA does not overexcite the nervous system and damage cells, but protects neurons. PEA doesn’t deplete neurotransmitter levels, it regulates them. This avoids the “crashing upon cessation of use” that is common with stimulant drugs.

Feelings of Happiness, Pleasure, and Emotional Wellbeing

PEA is an immediate shot of “happiness, pleasure, and emotional wellbeing,” even during stressful times. PEA increases the release and activity of dopamine, which is associated with the pleasure system of the brain and considered a “feel-good” neuro-modulator/neuro-transmitter-it activates a feeling of pleasure and euphoric sense of wellbeing.

Increased Energy, Alertness, and Sensory Perception

The boost of energy-generating catecholamines (dopamine and noradrenalin) produces amphetamine-like stimulation and performance enhancement. PEA induces behavioral and physiological effects similar to those of amphetamine. Unlike amphetamine and other stimulant drugs, PEA is endogenous to the brain. PEA does not develop tolerance or dependency, or produce any side effects. PEA has been referred to by researchers as an “endogenous amphetamine” because it is produced by the brain. After ingesting PEA, people commonly report a surge of energy, wakefulness, alertness, and heightened senses.

Increased Cognitive Power and Smartness

PEA helps upgrade your mind with faster thinking, increased attention, quicker decision making, greater sensory awareness, less brain fog, and immediate, easy memory access. PEA releases acetylcholine, a neurotransmitter that plays an integral role in learning and memory. Brain receptors respond to acetylcholine by facilitating memory and higher cognitive functions. In addition, PEA increases noradrenalin, the brain’s version of adrenaline, which is required for alertness, concentration, and “get up and go.” An increase in glutamate from PEA can throw switches to the “on” position in memory-forming circuits, making it easier to form memories.

Help for Attention Disorders, Addictions, and Substance Abuse

Current research on PEA trace amine receptor neuro-modulator and neurotransmitter actions is reaping rewards. PEA is proving beneficial for attenuating attention-related problems, controlling addictions, overcoming substance abuse, and correcting neurobehavioral problems. This is an exciting area of research for PEA with many practical uses and clinical implications.

Proven Mood-Brightener and Relief of Depression

The “Phenylethylamine Hypothesis of Depression” states that PEA sustains psychological energy just as thyroid hormone sustains physical energy. And a deficit of PEA produces depression. The Phenylethylamine hypothesis goes on to state that PEA is a neuro-modulator of mood, attention, pleasure-seeking behavior, and libido. Scientist tell us that a deficit in the brain content of PEA and/or a decrease in the turnover of endogenous PEA is causal factor in subclinical and clinical depressive conditions. Taking PEA orally to replace and increase PEA brain levels may dispatch the symptoms. It gives individuals an elevation of mood and increased quality of life.

A Natural Internal NDRI and SSRI

PEA is a research-proven substance for quickly boosting a depressive mood of sadness, hopelessness, discouragement, and being “down in the dumps.” PEA is potent in enhancing the release of catecholamines and blocking their re-uptake, especially of dopamine. PEA has similar actions with serotonin, just not as powerful. That means that PEA is a strong NDRI (Norepinephrine-Dopamine Reuptake Inhibitor) and a weaker-acting SSRI (Selective Serotonin Reuptake Inhibitor). Their synergistic actions make PEA an ideal nutriceutical complement or alternative to standard protocols.

In terms of safety, PEA does produce the adverse effects of pharmaceutical NDRI’s and SSRI’s. This is due to PEA’s self-regulating control of neurotransmissions and its intrinsic neuro-protective properties.

Rapid Sustained Depression Relief in 60 Percent of Patients

In multiple clinical trials, PEA produced a rapid and sustained relief of depression in 60 percent of the patients after two weeks. In one trial, the patients were previously resistant to a wide range of treatments, including SSRI’s and MAOI’s. They began showing mood elevation within a day or two of taking PEA. Other reported effects included restoration of energy, concentration, motivation, and sex drive. PEA treatment improved their sleep and there were no side effects.

The success rate for treating depression with PEA is the same percentage as the major Serotonin-Selective Re-uptake Inhibitors (SSRI’s)-but without their serious side effects and toxicity. In fact, PEA has produced sustained relief of both acute and chronic depression in a significant number of people, including some who were unresponsive to standard protocols, according to research psychopharmacologist and psychiatrist Dr. Hector Sabelli.

Runner’s Euphoric High

Moderate exercise normally increases PEA levels, so researchers now believe that this increase causes the euphoric mood often called “runner’s high.” What about the natural substances called endorphins, previously linked to runner’s high? Endorphins don’t penetrate the brain, and when chemicals were administered to block the binding of endorphins to their neuron receptors, the runners still experienced euphoric high. Also, depressed people tend to have low PEA levels, so the researchers say there now is an explanation of why exercise is a natural antidepressant.

The Mediator of Psychological Energy, Love, Self-Love, and Libido

Freud developed the concept of a single psychobiological energy as the source of our mental, emotional, and sexual energy. This single energy is the driving force for sexual libido, pleasure-seeking behavior, interpersonal energy, love, warmth, affection, and other personal attributes. Modern research with PEA provides a neuro-physiological basis for Freud’s model of the 19th Century.

PEA actions on neurotransmissions have produced sexual arousal and erections in research studies. PEA is shown to create feeling of love, self-love, emotional warmth, and sexual pleasure. According to Dr. Hector Sabelli, who has extensively studied PEA, “I believe that PEA may be the hormone of libido,” not just testosterone. Sabelli’s research found that high PEA levels lead to increased sex drive, pleasure-seeking activity, and courage, while low levels reflect the loss of libido, physical drive, and emotions in depression. In short, PEA is a natural aphrodisiac.

Fat Burning and Weight Loss

PEA’s ability to elevate blood catecholamine levels may be useful in the thermogenic (heat-caused) burning of stored body fat for losing weight. Increased levels of epinephrine and norepinephrine can stimulate beta-adrenergic receptors located on adipose (fat) tissue to release fatty acids into circulation as a fuel source. In other words, PEA turns up one’s cellular thermostat to burn fat for energy. Plus, catecholamines act on hormone-sensitive lipase, the enzyme for removing fat from storage sites. In addition, PEA has demonstrated appetite-reducing activity, reducing food intake in animal research.

Supercharged Physical and Athletic Performance

PEA can increase physical energy, stamina, concentration, coordination, reaction and thinking time, spatial recognition, motivation, and confidence in most adults. PEA is a natural biochemical stimulant that increases actions of dopamine, norepinephrine, and serotonin neurotransmitters for better physical and mental performance.

PEA helps prevent the age-related gradual decline in physical activity and performance after reaching maturity. By raising catecholamine activity to youthful levels, PEA helps elevate the ceiling for “maximum physical performance.”

How PEA Works

When taken orally, PEA easily crosses the blood-brain barrier. It is rapidly available in the brain as an neuro-amplifier of neurotransmitter signal strength, a neuroregulator of transmitter transport, and an excitatory (stimulating) neurotransmitter in different region of the brain.

Amplifies Neurotransmitter Activity

PEA is released from nerve vesicles in the brain, causing a larger release of neurotransmitters in response to a given nerve signal. It’s like “cranking up the volume” of nerve cell activity. PEA induces higher concentration, continuous strong release, and greater activity of dopamine (for feeling pleasure and wellbeing), norepinephrine (the brain’s stimulant for “get-up-and-go”), acetylcholine (for memory and cognitive functions), and serotonin (for good moods and feelings, and impulse control).

Modulates Neurotransmitter Functions by Binding TAAR1

PEA modulates neuro-transporter functions by binding with its paired Trace Amine-Associated Receptor 1 (TAAR1). TAAR1 is a G-protein coupled receptor that is activated by PEA and certain monoamines. Activation of TAAR1 by PEA significantly inhibits the uptake and induces efflux of the neurotransmitters dopamine, norepinephrine, and serotonin. PEA increases the extracellular levels of these neurotransmitters by inhibiting their re-uptake into the pre-synaptic cell, and this increases their beneficial activity throughout the body.

A Guardian of Neurobiology and a Homeostatic Regulator Against Metabolic Dysfunctions

PEA is neural guardian of homeostasis (maintaining healthy metabolic equilibrium). The binding of PEA with TAAR1 protects delicate neural circuitry against harmful changes. PEA self-regulates transmitter activity to prevent over-excitation or under-stimulation transmitter signal strength and activity. PEA acts as an homeostatic controller to maintain the neuronal activity within defined physiological limits to prevent metabolic dysfunctions and neurological disorders. This makes PEA and other trace amines perfect candidates for the development of novel therapeutics for a wide range of human disorders.

Endogenous Amphetamine-Like Stimulating Neurotransmitters

PEA is an excitatory neurotransmitter with its own receptor and a chemical structure similar to amphetamines that induces behavioral and electrophysiological effects similar to those of amphetamine. Unlike amphetamine, PEA is endogenous to the brain and does not develop tolerance or dependency, or produce any side effects, such as amphetamines sold under the trade name Aderall® and the adverse effects of the popular drug stimulant Ritalin® that is prescribed for treating Attention Deficit Disorders.

Concentrated Limbic System Neurotransmitter

PEA is highly concentrated in the limbic system of the brain, the center of emotions. The interaction of PEA with its chemical receptor sends signals to the brain that can improve emotions, pleasurable feelings, motivation, physical drives, impulse control, social behavior, sexuality, creativity and sensory perceptions, the sense of wellbeing, and overall performance.

Trigger of Brain Plasticity and Neurogenesis

PEA may trigger neurotransmitters for “brain plasticity” and “neurogenesis” (the forming of new brain cells, information processing connections, and functions) that increase cognition, learning, memory, skills, smartness, and performance. The mechanism is thought to involve PEA’s action of increasing dopamine neurotransmitter from synapses and acting as a dopamine re-uptake inhibitor in certain brain regions.

Actions of PEA on Neurotransmitters

  • Stimulates dopamine’s nerve terminals and activity for feeling pleasure, libido and emotional wellbeing.
  • Increases epinephrine and norepinephrine catecholamine activity, for energy production and inhibition of their re-uptake.
  • Increases the action of acetylcholine for cognitive functions by stimulating the AMPA glutamatergic receptors.
  • Elevates mental alertness and mood by suppressing the inhibitory effects of GABA-B receptors.
  • Enhances serotonin release and its uplifting activity on mood, emotions, and control.

Furthermore, PEA self-regulates transmitter activity to prevent over-excitation or under-stimulation transmitter signal strength and activity. Thus PEA acts as an homeostatic controller to maintain the neuronal activity of monoamine neurotransmitters within defined physiological limits.

Present and Future Therapeutic Use

PEA may be therapeutically useful in any disorder associated with an alteration in the functioning of its partner neurotransmitters. In the case of PEA, it is primarily the transmitter’s dopamine, norepinephrine, serotonin, and acetylcholine. This gives PEA the ability to alleviate the symptoms of vast number of neurological dysfunctions and behavioral disorders without addressing the underlying pathology of the disease. Convincing evidence has been presented for using PEA in the treatment for a wide range of neurological dysfunctions and behavioral disorders, such as:

  • Affective disorders (depression, bipolar disorder)
  • Attention deficit / hyperactivity disorder
  • Cognitive dysfunction (brain fog, confusion, forgetfulness, poor concentration, a sluggish cognitive tempo, slowed reaction time, and diminished awareness)
  • Drug abuse and substance dependence (alcoholism, nicotine dependence, and addictions to methamphetamines, cocaine opioids, and psycho-stimulants)
  • Addictive behavior (gambling, sexual addiction)
  • Eating disorders (obesity, anorexia)

More Uplifting and Effective than Phenylalanine

The human brain forms PEA from the essential amino acid l-phenylalanine by an enzyme-driven cellular process. Phenylalanine is the precursor to the amino acid tyrosine, which produces the neurotransmitters dopamine, norepinephrine, and adrenalin in a sequential process, but phenylalanine supplements don’t significantly boost PEA concentrations. And phenylalanine supplements can boost catecholamine neurotransmitter levels excessively, producing anxiety, headaches, and hypertension. What’s worse, some people’s biochemistry transforms phenylalanine into the nasty, neurotoxic (brain-damaging) metabolites. By contrast, PEA safely increases and amplifies the activity of dopamine, norepinephrine, and other brain transmitters to produce desirable and remarkable effects.

Fast-Acting But Short-Lived

The human body can synthesize significant quantities of PEA, but functional levels of a PEA remain fairly low because it is usually broken down by the enzyme MAO-B within several hours. As result, PEA effects are relatively short-acting. So the fast-acting PEA compound is best taken by most people every 3-4 several hours for an immediate boost and for maintaining activity throughout the day.

Bioperine, a Natural Bioavailability Enhancer of PEA

Bioperine® is a patented standardized extract that contains 95 percent Piperine, a phytochemical that enhances the bioavailability of PEA. Piperine increases absorption from the gut and inhibits MAO-B from breaking down dopamine, with mood-brightening effects. The synergy between Bioperine and PEA can increase and extend the effects of PEA.

Protected Patent-pending Nanosphere Delivery

PEA is best formulated with a patent-pending “Self-Emulsifying Nanosphere Delivery System.” Natural phospholipids and medium-chain triglycerides form a nanosphere protective covering in the intestinal tract, enhancing bioavailability (delivery) of PEA. PEA is manufactured in protective-coated tablets that safeguard PEA from degradation in the harsh acidic environment of the stomach and carry PEA to the intestinal tract. PEA is rapidly released for PEA intestinal absorption, enhanced delivery to the bloodstream and transport to the brain.

Warnings: Do not use PEA if you are pregnant or nursing. Do not take PEA if you have used an MAO inhibitor such as isocarboxazid (Marplan), phenelzine (Nardil), rasagiline (Azilect), or tranylcypromine (Parnate) within the past 14 days, as MAO inhibitors prolong and increase the actions of phenylethylamine. Do not take PEA if have phenylketonuria (PKU). If you are on medication or have a health condition, consult a physician before using PEA.

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Author: Richard Clark Kaufman, PhD